Tetracycline

 Pharmacology of Tetracycline

Introduction 

    Tetracycline, sold under the brand name Sumycin among others, is an oral antibiotic in the tetracyclines family of medications, used to treat a number of infections, including acne, cholera, brucellosis, plague, malaria, and syphilis. Common side effects include vomiting, diarrhea, rash, and loss of appetite. 

Formula: C₂₂H₂₄N₂O₈

IUPAC ID: (4S,6S,12aS)-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxonaphthacene-2-carboxamide

Molar mass: 444.435 g/mol

CAS ID: 60-54-8

Elimination half-life: 8–11 hours, 57–108 hours (kidney impairment)

Metabolism: Not metabolized

DOSAGES OF TETRACYCLINE

Capsule/Tablet

• 250 mg
• 500 mg

Syrup (extemporaneously prepared)

• 125mg/5mL
• 5 mg

Dosage Considerations – Should be Given as Follows:

Chronic Bronchitis, Acute Exacerbation

• 500 mg orally every 6 hours

Acne

• 250-500 mg orally every 12 hours

Ehrlichiosis

• 500 mg orally every 6 hours for 7-14 days

Vibrio Cholera

• Adult: 500 mg orally every 6 hours for 3 days
• Pediatric, Single dose: 25 mg/kg orally; not to exceed 1 g/dose
• Pediatric, Multiple dose: 40 mg/kg/day orally divided every 6 hours for 3 days; not to exceed 2 g/day

Malaria, Severe Treatment (Unlabeled)

• Adult: 500 mg orally every 6 hours for 7 days with quinidine gluconate
• Children under 8 years: Not recommended; tooth discoloration and enamel hypoplasia may occur with use in young children
• Children over 8 years: 25-50 mg/kg/day orally divided every 6 hours, not to exceed 250 mg/dose every 6 hours for 7 days with quinidine gluconate

Dosage Modifications

Renal impairment

• CrCl 50-80 mL/min: Dose frequency every 8-12 hours
• CrCl 10-50 mL/min: Dose frequency every 12-24 hours
• CrCl less than 10 mL/min: Dose frequency every 24 hours

Dosing Considerations

Susceptible organisms

• Acinetobacter spp, Actinomyces israelii, Afipia felis, Bacillus anthracis, Bacteroides spp, Bartonella bacilliformis, Bartonella quintana, Bordetella pertussis, Borrelia recurrentis, Brucella spp, Capnocytophaga canimorsus, Campylobacter jejuni, Chlamydia spp, Citrobacter spp, Coxiella burnetii, Eikenella corrodens, Escherichia coli, Francisella tularensis, Leptospira interrogans, Helicobacter pylori, Klebsiella spp, Listeria monocytogenes, Moraxella catarrhalis, Mycoplasma pneumoniae, Neisseria gonorrhoeae, Propionibacterium acnes, Rickettsiae, Shigella spp, Staphylococcus aureus, Streptococcus pneumoniae, Treponema pallidum, Ureaplasma urealyticum, Vibrio cholerae, Yersinia pestis, Yersinia enterocolitica, Yersinia pseudotuberculosis

General Dosing Guidelines, pediatric

• Children under 8 years: Not recommended; tooth discoloration and enamel hypoplasia may occur with use in young children
• Children over 8 years: 25-50 mg/kg/day orally divided every 6 hours; not to exceed 3 g/day

Administration

• Take on empty stomach; do not take with dairy product

WHAT ARE SIDE EFFECTS ASSOCIATED WITH USING TETRACYCLINE?

Common side effects of tetracycline include:

• Discoloration of teeth and enamel hypoplasia (young children)
• Diarrhea
• Nausea
• Photosensitivity
• Stomach upset
• Loss of appetite
• White patches or sores inside your mouth or on your lips
• Swollen tongue
• Black hairy tongue
• Sore throat
• Trouble swallowing
• Dizziness
• Headache
• Sores or swelling in your rectal or genital area
• Vaginal itching or discharge

Less common side effects of tetracycline include:

• Abdominal cramps
• Antibiotic-associated pseudomembranous colitis
• Bulging fontanels in infants
• Diabetes insipidus syndrome
• Esophagitis
• Exfoliative dermatitis
• Increased intracranial pressure
• Itching
• Loss of appetite
• Pancreatitis
• Pericarditis
• Pigmentation of nails
• Pseudotumor cerebri
• Vomiting

Serious side effects of tetracycline include:

• Sunburn (sun sensitivity)
• Muscle pain
• Changes in the amount of urine
• Brown or gray tooth discoloration
• Numbness or tingling of the hands or feet
• Unusual fatigue
• New signs of infection (e.g., persistent sore throat, fever, chills)
• Hearing changes (e.g., ringing in the ears, decreased hearing)
• Easy bruising or bleeding
• Severe stomach or abdominal pain
• Yellowing eyes or skin
• Dark urine

This is not a complete list of side effects and other serious side effects may occur. Call your doctor for information and medical advice about side effects. You may report side effects to any nearby standard hosptal.

WHAT OTHER DRUGS INTERACT WITH TETRACYCLINE?

If your doctor has directed you to use this medication for your condition, your doctor or pharmacist may already be aware of any possible drug interactions or side effects and may be monitoring you for them. Do not start, stop, or change the dosage of this medicine or any medicine before getting further information from your doctor, healthcare provider or pharmacist first.

Severe Interactions of tetracycline include:

1. acitretin
2. flibanserin
3. lomitapide
4. tretinoin

Tetracycline has serious interactions with at least 71 different drugs.

Tetracycline has moderate interactions with at least 46 different drugs.

Tetracycline has mild interactions with at least 26 different drugs.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

WHAT ARE WARNINGS AND PRECAUTIONS FOR TETRACYCLINE?

Warnings

This medication contains tetracycline. Do not take Sumycin, Actisite, or Achromycin V if you are allergic to tetracycline or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Documented hypersensitivity
• Severe hepatic dysfunction

Effects of Drug Abuse

• No information available

Short-Term Effects

• See "What Are Side Effects Associated with Using Tetracycline?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Tetracycline?"

Cautions

• Photosensitivity may occur with prolonged exposure to sunlight or tanning equipment.
• Reduce dose in renal impairment.
• Consider drug serum level determinations in prolonged therapy.
• Tetracycline use during tooth development (last half of pregnancy through age 8 years) can cause permanent discoloration of teeth.
• Fanconilike syndrome may occur with outdated tetracyclines.
• Intravenous/intramuscular (IV/IM) no longer commercially available.

Pregnancy and Lactation

• Use systemic tetracycline during pregnancy only in LIFE-THREATENING emergencies when no safer drug is available. There is positive evidence of human fetal risk.
• Use periodontal fiber tetracycline with caution during pregnancy if benefits outweigh risks. Animal studies show risk and human studies are not available or neither animal nor human studies were done.
• Tetracycline use during tooth development (last half of pregnancy through age 8 years) can cause permanent discoloration of teeth.